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Glycoprotein Hormone Long-Acting Superagonists

a glycoprotein hormone and superagonist technology, applied in the direction of peptides, drug compositions, peptides, etc., can solve the problems of insufficient success in further modification of glycoprotein hormones to increase half-life and improve bioavailability

Active Publication Date: 2014-12-18
TROPHOGEN INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The patent text describes a modified version of a glycoprotein hormone that has increased efficacy compared to the natural version. This increased efficacy can be measured using various techniques. The increased efficacy can vary slightly from assay to assay or cell line to cell line, but it is consistent within a given assay or cell line. Overall, the modified hormone is more effective in its function.

Problems solved by technology

However, previous attempts to further modify glycoprotein hormones to increase half-life and improve bioavailability have been less than satisfactory and instead the modified glycoprotein hormones demonstrated only an attenuated response.

Method used

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  • Glycoprotein Hormone Long-Acting Superagonists
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  • Glycoprotein Hormone Long-Acting Superagonists

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examples

Design of Alpha Subunit Analogs

[0081]A human FSH superagonist glycoprotein with modifications to the α-subunit at Q13R+E14R+P16R+Q20R (human 4R) with a wild-type β-subunit demonstrated significant binding superiority over their wild-type counterparts.

[0082]Table 1 shows a comparison of human alpha wild-type (WT) and selected hFSH superagonists primary amino acid structure. N-terminal portions of human alpha wild-type (amino acid residues 1-28 of 92 total residues) and mutated forms are shown. Location of 4 superagonist substitutions to arginine (R) is in the shaded area. Selected 4 different inserts introducing one or two additional N-linked carbohydrate chains are marked between amino acid D3 and Q5 of the wild-type sequence.

TABLE 1WTTR4401 (4R)TR44701 (4R + Ins1)TR44601 (4R + Ins2)TR44201 (4R + Ins3)TR44301 (4R + Ins4)

[0083]The segments in Table 1 are listed as the following: SEQ ID NO: 43: hFSH WT; SEQ ID NO: 33, hFSH alpha (4R); SEQ ID NO: 34, hFSH alpha (4R+Ins1); SEQ ID NO: 35...

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Abstract

This invention provides long-acting, superactive analogs of glycoprotein hormones demonstrating enhanced bioactivity both in vitro and in vivo as compared to wild type counterparts. The analogs are particularly useful for treating subjects showing low receptor expression or poor receptor responsiveness, and for the treatment of any condition associated with glycoprotein hormone activity.

Description

SEQUENCE LISTING INFORMATION[0001]A computer readable text file, entitled “056815-5010-01-SequenceListing.txt,” created on or about Jun. 19, 2014 with a file size of about 30 kb contains the sequence listing for this application and is hereby incorporated by reference in its entirety.FIELD OF INVENTION[0002]This invention relates generally to modified glycoprotein hormones having superagonist activity, and the use thereof in the treatment of conditions associated with glycoprotein hormone activity. More specifically, this invention relates to modified glycoprotein molecules containing amino acid substitutions and one or more inserted peptides in the alpha subunit as compared to wild type alpha subunit, wherein such modified molecules exhibit enhanced pharmacological properties as compared to wild type glycoproteins.BACKGROUND OF INVENTION[0003]The gonadotropins follitropin (follicle-stimulating hormone, FSH) and chorionic gonadotropin, (CG), lutropin (luteinizing hormone, LH), and t...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): C07K14/59
CPCC07K14/59A61P15/08A61P5/00A61P5/06A61P5/24A61K38/24A61K38/00
Inventor SZKUDLINSKI, MARIUSZ W.WEINTRAUB, BRUCE D.
Owner TROPHOGEN INC
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